Assay Detail
Binding
CHEMBL3782873
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Inhibition of human recombinant MAOA expressed in Pichia pastoris preincubated for 15 mins measured after 30 mins by bioluminescent-coupled assay
15
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a Novel Inhibitor of Histone Lysine-Specific Demethylase 1A (KDM1A/LSD1) as Orally Active Antitumor Agent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.65 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3780674 | — | — | 1 | 7.60 |
| CHEMBL3780524 | — | — | 1 | 7.53 |
| CHEMBL3546846 | — | — | 1 | 7.51 |
| CHEMBL3780391 | — | — | 1 | 7.40 |
| CHEMBL3781329 | — | — | 1 | 7.26 |
| CHEMBL3780374 | — | — | 1 | 7.04 |
| CHEMBL3781124 | — | — | 1 | 6.80 |
| CHEMBL3780542 | — | — | 1 | 6.71 |
| CHEMBL3781125 | — | — | 2 | 6.54 |
| CHEMBL3781885 | — | — | 1 | 6.46 |
| CHEMBL3781494 | — | — | 1 | 6.23 |
| CHEMBL3780774 | — | — | 1 | 6.16 |
| CHEMBL3781560 | — | — | 1 | 6.00 |
| CHEMBL3781751 | IADADEMSTAT | 2.0 | 1 | 4.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3780674 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3780524 | — | IC50 | = | 29.7 | nM | 7.53 |
| CHEMBL3546846 | — | IC50 | = | 31.2 | nM | 7.51 |
| CHEMBL3780391 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3781329 | — | IC50 | = | 54.8 | nM | 7.26 |
| CHEMBL3780374 | — | IC50 | = | 90.5 | nM | 7.04 |
| CHEMBL3781124 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3780542 | — | IC50 | = | 193.1 | nM | 6.71 |
| CHEMBL3781125 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3781885 | — | IC50 | = | 344.7 | nM | 6.46 |
| CHEMBL3781494 | — | IC50 | = | 589.6 | nM | 6.23 |
| CHEMBL3780774 | — | IC50 | = | 687.1 | nM | 6.16 |
| CHEMBL3781125 | — | IC50 | = | 726.3 | nM | 6.14 |
| CHEMBL3781560 | — | IC50 | = | 999.8 | nM | 6.00 |
| CHEMBL3781751 | IADADEMSTAT | IC50 | = | 48380.0 | nM | 4.32 |